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G protein coupled receptors

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https://www.readbyqxmd.com/read/28737723/role-of-g-protein-coupled-receptors-in-the-regulation-of-structural-plasticity-and-cognitive-function
#1
REVIEW
Crystal C Y Leung, Yung H Wong
Cognition and other higher brain functions are known to be intricately associated with the capacity of neural circuits to undergo structural reorganization. Structural remodelling of neural circuits, or structural plasticity, in the hippocampus plays a major role in learning and memory. Dynamic modifications of neuronal connectivity in the form of dendritic spine morphology alteration, as well as synapse formation and elimination, often result in the strengthening or weakening of specific neural circuits that determine synaptic plasticity...
July 24, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28736556/ras-signaling-inhibitors-attenuate-disease-in-adjuvant-induced-arthritis-via-targeting-pathogenic-antigen-specific-th17-type-cells
#2
Morad Zayoud, Victoria Marcu-Malina, Einav Vax, Jasmine Jacob-Hirsch, Galit Elad-Sfadia, Iris Barshack, Yoel Kloog, Itamar Goldstein
The Ras family of GTPases plays an important role in signaling nodes downstream to T cell receptor and CD28 activation, potentially lowering the threshold for T-cell receptor activation by autoantigens. Somatic mutation in NRAS or KRAS may cause a rare autoimmune disorder coupled with abnormal expansion of lymphocytes. T cells from rheumatoid arthritis (RA) patients show excessive activation of Ras/MEK/ERK pathway. The small molecule farnesylthiosalicylic acid (FTS) interferes with the interaction between Ras GTPases and their prenyl-binding chaperones to inhibit proper plasma membrane localization...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28736254/bisphenol-a-affects-trophoblast-invasion-by-inhibiting-cxcl8-expression-in-decidual-stromal-cells
#3
Xiaoqian Li, Yina Wang, Pu Wei, Dongyan Shi, Shuang Wen, Fengjiao Wu, Lixin Liu, Ninghe Ye, Hong Zhou
Bisphenol A (BPA), an environmental endocrine-disrupting organic chemical, has been positively associated with the rate of implantation failure of in vitro fertilization. However, the underlying mechanisms remain unclear. To reveal the impact and the underlying mechanism of BPA on the crosstalk between trophoblast and decidual stromal cells (DSCs), we determined whether BPA was able to affect trophoblast invasion in vitro. We found that BPA significantly inhibited CXCL8 expression in DSCs, which hindered trophoblast invasion, and activated the phosphorylation of ERK in DSCs...
July 20, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28736033/acid-sensing-t-cell-death-associated-gene-8-receptor-expression-in-panic-disorder
#4
Jeffrey R Strawn, Lauren L Vollmer, Katherine M J McMurray, Jeffrey A Mills, Sarah A Mossman, Sara T Varney, Heidi K Schroeder, Renu Sah
BACKGROUND: While disruption of acid-base homeostasis has been pathoetiologically implicated in panic disorder (PD), the mechanism by which pH imbalance is translated to panic pathophysiology is poorly understood. Recently, in a translational rodent model of PD, we reported a role of microglial acid sensing G-protein coupled receptor, T cell death associated gene-8 (TDAG8) in panic-associated behavior and physiology. However, the clinical validity of the TDAG8 receptor has not been investigated...
July 20, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28735625/free-fatty-acid-receptor-ffar-agonists-inhibit-proliferation-of-human-ovarian-cancer-cells
#5
Mandi M Hopkins, Kathryn E Meier
Many cellular actions of omega-3 fatty acids are mediated by two G protein-coupled receptors, FFA1 and FFA4, free fatty acid receptor (FFAR) family members that are activated by these dietary constituents. FFAR agonists inhibit proliferation of human prostate and breast cancer cells. Since omega-3 fatty acids can inhibit ovarian cancer cell growth, the current study tested the potential role of FFARs in the response. OVCAR3 and SKOV3 human ovarian cancer cell lines express mRNA for FFA1; FFA4 mRNA was detected at low levels in SKOV3 but not OVCAR3...
July 2017: Prostaglandins, Leukotrienes, and Essential Fatty Acids
https://www.readbyqxmd.com/read/28734639/ffa4-gpr120-pharmacology-and-therapeutic-opportunities
#6
REVIEW
Graeme Milligan, Elisa Alvarez-Curto, Brian D Hudson, Rudi Prihandoko, Andrew B Tobin
Free Fatty Acid receptor 4 (FFA4), also known as GPR120, is a G-protein-coupled receptor (GPCR) responsive to long-chain fatty acids that is attracting considerable attention as a potential novel therapeutic target for the treatment of type 2 diabetes mellitus (T2DM). Although no clinical studies have yet been initiated to assess efficacy in this indication, a significant number of primary publications and patents have highlighted the ability of agonists with potency at FFA4 to improve glucose disposition and enhance insulin sensitivity in animal models...
July 19, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28734238/decreased-levels-of-g-protein-coupled-estrogen-receptor-in-children-with-autism-spectrum-disorders
#7
Hatice Altun, Ergül Belge Kurutaş, Nilfer Şahin, Hayati Sınır, Ebru Fındıklı
Sex hormones, specially estrogen, and ıt is receptors plays a critical role in the pathogenesis of psychiatric disorders including autism spectrum disorders (ASD). The aim of this study was to investigate the relationship between ASD and G protein-coupled estrogen receptor (GPER), a recently discovered estrogen receptors, and also to study the relation of serum GPER levels with the severity of autistic symptoms. The present study included 45 children with drug naive ASD diagnosed by DSM-V criteria, aged between 3 and 12 years and 40 age- and gender-matched healthy controls...
June 6, 2017: Psychiatry Research
https://www.readbyqxmd.com/read/28733900/the-putative-role-of-environmental-mercury-in-the-pathogenesis-and-pathophysiology-of-autism-spectrum-disorders-and-subtypes
#8
REVIEW
G Morris, B K Puri, R E Frye, M Maes
Exposure to organic forms of mercury has the theoretical capacity to generate a range of immune abnormalities coupled with chronic nitro-oxidative stress seen in children with autism spectrum disorder (ASD). The paper discusses possible mechanisms explaining the neurotoxic effects of mercury and possible associations between mercury exposure and ASD subtypes. Environmental mercury is neurotoxic at doses well below the current reference levels considered to be safe, with evidence of neurotoxicity in children exposed to environmental sources including fish consumption and ethylmercury-containing vaccines...
July 22, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28733525/ackr3-expression-on-diffuse-large-b-cell-lymphoma-is-required-for-tumor-spreading-and-tissue-infiltration
#9
Viola Puddinu, Sabrina Casella, Egle Radice, Sylvia Thelen, Stefan Dirnhofer, Francesco Bertoni, Marcus Thelen
Diffuse large B cell lymphoma (DLBCL) is the most frequent lymphoma accounting for more than the 30% of the cases. Involvement of extranodal sites, such as bone marrow and central nervous system, is associated with poor prognosis. A contribution of the chemokine system in these processes is assumed as it is known as a critical regulator of the metastatic process in cancer. The atypical chemokine receptor 3 (ACKR3), which does not couple to G-proteins and does not mediate cell migration, acts as a scavenger for CXCL11 and CXCL12, interfering with the tumor homing CXCL12/CXCR4 axis...
June 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28733475/gper-modulates-tone-and-coronary-vascular-reactivity-in-male-and-female-rats
#10
Angelina Rafaela Debortoli, Wender do Nascimento Rouver, Nathalie Tristão Banhos Delgado, Vinicius Mengal, Erick Roberto Gonçalves Claudio, Laena Pernomian, Lusiane Maria Bendhack, Margareth Ribeiro Moysés, Roger Lyrio Dos Santos
Compared with age-matched men, premenopausal women are largely protected from coronary artery disease, a difference that is lost after menopause. The effects of oestrogens are mediated by the activation of nuclear receptors (ERα and ERβ) and by the G protein-coupled oestrogen receptor (GPER). This study aims to evaluate the potential role of GPER in coronary circulation in female and male rats. The baseline coronary perfusion pressure (CPP) and the concentration-response curve with a GPER agonist (G-1) were evaluated in isolated hearts before and after the blockade of GPER...
August 2017: Journal of Molecular Endocrinology
https://www.readbyqxmd.com/read/28733085/functional-consequences-of-chemically-induced-%C3%AE-arrestin-binding-to-chemokine-receptors-cxcr4-and-ccr5-in-the-absence-of-ligand-stimulation
#11
Marcel Liebick, Sarah Henze, Viola Vogt, Martin Oppermann
Chemokine receptor signaling is a tightly regulated process which was for a long time exclusively attributed to heterotrimeric G proteins. β-Arrestins constitute a separable signaling arm from classical heterotrimeric G proteins, in addition to their well-established roles in receptor desensitization and endocytosis. In order to clearly dissect β-arrestin- from G protein-dependent effects we forced the recruitment of β-arrestin to CXCR4 and CCR5 independently of agonist-promoted receptor activation through chemically-induced dimerization...
July 18, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28733084/reciprocal-regulation-of-%C3%AE-2-adrenoceptor-activated-camp-response-element-binding-protein-signalling-by-arrestin2-and-arrestin3
#12
Alexander Pearce, Lucy Sanders, Paul J Brighton, Shashi Rana, Justin C Konje, Jonathon M Willets
Activation of Gs coupled receptors (e.g. β2-adrenoreceptor (β2AR)) expressed within the uterine muscle layer (myometrium), promotes intracellular cAMP generation, inducing muscle relaxation through short-term inhibition of contractile proteins, and longer-term modulation of cellular phenotype to promote quiescence. In the myometrium cAMP-driven modulation of cell phenotype is facilitated by CREB activity, however despite the importance of CREB signalling in the promotion of myometrial quiescence during pregnancy, little is currently known regarding the molecular mechanisms involved...
July 18, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28731695/how-rhodopsin-tunes-the-equilibrium-between-protonated-and-deprotonated-forms-of-the-retinal-chromophore
#13
Siri Camee van Keulen, Alicia Solano, Ursula Rothlisberger
Rhodopsin is a photoactive G-protein-coupled receptor (GPCR) that converts dim light into a signal for the brain, leading to eyesight. Full activation of this GPCR is achieved after passing through several steps of the protein's photoactivation pathway. Key events of rhodopsin activation are the initial cis-trans photoisomerisation of the covalently bound retinal moiety followed by conformational rearrangements and deprotonation of the chromophore's protonated Schiff base (PSB), which ultimately lead to full activation in the meta II state...
July 21, 2017: Journal of Chemical Theory and Computation
https://www.readbyqxmd.com/read/28731171/protective-role-of-pollen-typhae-total-flavone-against-the-palmitic-acid-induced-impairment-of-glucose-stimulated-insulin-secretion-involving-gpr40-signaling-in-ins-1-cells
#14
Xiao-Tao Feng, Hui-Ming Duan, Shuang-Lei Li
Prolonged elevated levels of free fatty acids (FFAs) contribute to the impairment of insulin secretion function of pancreatic β cells, a hallmark of type 2 diabetes, which is partly attributed to the dysfunction of G-protein-coupled receptor 40 (GPR40) signaling. Pollen Typhae total flavone (PTF), an extract from a Chinese herbal medicine named Pollen Typhae, has been reported to effectively treat type 2 diabetes, but the underlying mechanisms remain to be fully elucidated. In the present study, palmitic acid (PA), a saturated fatty acid, severely impaired glucose-stimulated insulin secretion (GSIS) in a time-dependent manner in INS-1 cells, and PTF treatment prevented the impairment in a dose-dependent manner...
July 18, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28731148/molecular-genetics-and-targeted-therapy-of-wnt-related-human-diseases-review
#15
Masuko Katoh, Masaru Katoh
Canonical WNT signaling through Frizzled and LRP5/6 receptors is transduced to the WNT/β-catenin and WNT/stabilization of proteins (STOP) signaling cascades to regulate cell fate and proliferation, whereas non-canonical WNT signaling through Frizzled or ROR receptors is transduced to the WNT/planar cell polarity (PCP), WNT/G protein-coupled receptor (GPCR) and WNT/receptor tyrosine kinase (RTK) signaling cascades to regulate cytoskeletal dynamics and directional cell movement. WNT/β-catenin signaling cascade crosstalks with RTK/SRK and GPCR-cAMP-PKA signaling cascades to regulate β-catenin phosphorylation and β-catenin-dependent transcription...
July 19, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28730837/molecular-basis-of-trpa1-regulation-in-nociceptive-neurons-a-review
#16
A Kádková, V Synytsya, J Krusek, L Zímová, V Vlachová
Transient receptor potential A1 (TRPA1) is an excitatory ion channel that functions as a cellular sensor, detecting a wide range of proalgesic agents such as environmental irritants and endogenous products of inflammation and oxidative stress. Topical application of TRPA1 agonists produces an acute nociceptive response through peripheral release of neuropeptides, purines and other transmitters from activated sensory nerve endings. This, in turn, further regulates TRPA1 activity downstream of G-protein and phospholipase C-coupled signaling cascades...
July 18, 2017: Physiological Research
https://www.readbyqxmd.com/read/28730831/the-galanin-and-galanin-receptor-subtypes-its-regulatory-role-in-the-biological-and-pathological-functions
#17
J Šípková, I Kramáriková, S Hynie, V Klenerová
The multitalented neuropeptide galanin was first discovered 30 years ago but initially no biologic activity was found. Further research studies discovered the presence of galanin in the brain and some peripheral tissues, and galanin was identified as a modulator of neurotransmission in the central and peripheral nervous system. Over the last decade there were performed very intensive studies of the neuronal actions and also of nonneuronal actions of galanin. Other galanin family peptides have been described, namely galanin, galanin-like peptide, galanin-message associated peptide and alarin...
July 18, 2017: Physiological Research
https://www.readbyqxmd.com/read/28729619/effects-of-4-1h-quinolinone-derivative-a-novel-non-nucleotide-allosteric-purinergic-p2y-2-agonist-on-cardiomyocytes-in-neonatal-rats
#18
Kensuke Sakuma, Hideyuki Nakagawa, Tatsuo Oikawa, Masakuni Noda, Shota Ikeda
Purinergic P2Y 2 receptors, G-protein coupled receptors that primarily couple with Gαq/11-proteins, are activated equipotently by adenosine-5'-triphosphate (ATP) and uridine-5'-triphosphate. Evidence suggests that P2Y 2 agonists make potential drug candidates for the treatment of cardiovascular diseases. However, selective non-nucleotide, small-molecule P2Y 2 agonists have yet to be developed. In this report, we discuss Compound 89, a novel non-nucleotide allosteric P2Y 2 agonist that was active in signal transduction and gene induction, and in our in vitro cardiac hypertrophy model...
July 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28729439/striatal-gpr88-modulates-foraging-efficiency
#19
Aundrea Rainwater, Elisenda Sanz, Richard D Palmiter, Albert Quintana
The striatum is anatomically and behaviorally implicated in behaviors that promote efficient foraging. To investigate this function, we studied instrumental choice behavior in mice lacking GPR88, a striatum-enriched orphan G-protein-coupled receptor that modulates striatal medium spiny neuron (MSN) excitability. Our results reveal that hungry mice lacking GPR88 (KO mice) were slow to acquire food-reinforced lever-press, but could lever press similar to controls on a progressive-ratio schedule. Both WT and KO mice discriminated between reward and no-reward levers; however, KO mice failed to discriminate based on relative quantity- reward (1 versus 3 food pellets) or effort (3 versus 9 lever presses)...
July 20, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28728843/expression-and-prognostic-role-of-orphan-receptor-gpr110-in-glioma
#20
Haiping Shi, Shiyuan Zhang
Glioma is the most common type of malignancy in the central nervous system, which has a poor prognosis due to its rapid progression and diffuse invasion. Identification of novel biomarkers for glioma would be invaluable for studying disease mechanism and improving prognosis. Orphan G protein-coupled receptor 110 (GPR110) belongs to the subfamily VI of adhesion GPCR. The knowledge of the ligand, signaling pathway or physiology function of GPR110 is poorly elucidated. The potential role of GPR110 as an oncogene in mouse has been recently reported by mutagenesis screen...
July 17, 2017: Biochemical and Biophysical Research Communications
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